The fluorescent molecule capable of recognizing 10-hydroxycamptothecin (HCPT), a broad-spectrum anti-tumor drug, is not only able to detect it, but also able to enhance its activity due to the improvement of the delivery. Therefore, the construction of highly selective fluorescent hosts of HCPT is valuable, but remains challenging. In this work, an amphiphilic carbazole macrocyclic molecule (3) was synthesized and the host-guest interaction between 3 and HCPT was studied by fluorescence spectroscopy, NMR, scanning electron microscopy and transmission electron microscopy. The results showed that 3 could recognize HCPT with a stoichiometric ratio of 2∶1 via the mechanism of fluorescence resonance energy transfer (FRET) and a binding constant of 1.26×10¹⁴ (mol/L)^－2. The detection of limit (LOD) is 11.7 nmol•L^－1. In addition, the complexation enhanced the activity of HCPT to inhibit the proliferation of MCF-7 (Michigan Cancer Foundation-7) cells in vitro, and the IC₅₀ value decreased by two orders of magnitude, indicating that 3 possessed the dual function of both fluorescence probe and molecular carrier, thus providing scientific basis for further research.